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At least three rings in the polycyclo ring system

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514247000 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)

514248000 - Polycyclo ring system having a 1,2- or 1,4-diazine as one of the cyclos

514249000 - 1,4-diazine as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514251000 Isoalloxazine (e.g., riboflavins, Vitamin B2, etc.) 7
Entries
DocumentTitleDate
20090215788Pyrrolopyrazine kinase inhibitors - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I,08-27-2009
20130029997PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia;01-31-2013
20100137327NOVEL SEMICARBAZIDE AND CARBONYLHYDRAZIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel semicarbazide and carbonylhydrazide derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels.06-03-2010
20090239874Pyrido[3,2-e]pyrazines, their use as inhibitors of phospohodiesterase 10, and processes for preparing them - The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.09-24-2009
20110195971Methods of identifying responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites: dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or said patient has hypertriglyceridemai and/or hypertension . The present invention is also directed to treating identified patients with dopamine agonist therapy.08-11-2011
20110195970Methods of identifying and treating responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites: dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or fasting triglycerides are greater than about 150 mg/dl and/or said patient has hypertension. The present invention is also directed to treating identified patients with dopamine agonist therapy.08-11-2011
20100081663METHOD OF THERAPEUTIC ADMINISTRATION OF DHE TO ENABLE RAPID RELIEF OF MIGRAINE WHILE MINIMIZING SIDE EFFECT PROFILE - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C04-01-2010
20130210830THERAPEUTIC COMPOSITIONS - The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.08-15-2013
20100075973POLO-LIKE KINASE INHIBITORS - The present invention provides PLK inhibitors of the formula03-25-2010
20100075974HETEROCYCLIC GPR40 MODULATORS - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I:03-25-2010
20120245179Method Of Therapeutic Administration of DHE To Enable Rapid Relief Of Migraine While Minimizing Side Effect Profile - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C09-27-2012
20130035341MACROCYCLIC INTEGRASE INHIBITORS - Compound having formula I02-07-2013
20130040957Deuterium-Enriched Pyrimidine Compounds and Derivatives - The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof,02-14-2013
20090176791Diaryl Ureas for Treating Pulmonary Hypertension - The present invention relates to pharmaceutical compositions for treating, preventing or managing pulmonary hypertension comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound.07-09-2009
20120208822PYRIMIDO-PYRROLO-QUINOXALINEDIONE INHIBITORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN AND USES THEREFOR - Provided herein are pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity. The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, polycystic kidney disease. The compounds may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.08-16-2012
20110003824Caspase Inhibitors and Uses Thereof - This invention provides novel caspase inhibitors of formula I:01-06-2011
20090325971Pentacyclic Alkaloid Compounds and Methods of Use Thereof - The present invention relates to Pentacyclic Alkaloid Compounds, compositions comprising an effective amount of a Pentacyclic Alkaloid Compound and methods for treating or preventing cancer, a bacterial infection, a fungal infection, or a yeast infection, comprising administering to a subject in need thereof an effective amount of a Pentacyclic Alkaloid Compound. The present invention also relates to compounds and methods that are useful for making Cribrostatin IV.12-31-2009
20090306089COMPOUNDS - Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof:12-10-2009
20090093489NOVEL COMPOUNDS FOR TREATMENT OF CANCER AND DISORDERS ASSOCIATED WITH ANGIOGENESIS FUNCTION - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.04-09-2009
20110015201HEDGEHOG PATHWAY ANTAGONISTS AND METHODS OF USE - The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.01-20-2011
20080293729COMPOSITION AND METHOD OF DECREASING RENAL ISCHEMIC DAMAGE - A method of decreasing renal ischemic damage comprising a) identifying an organism having a kidney that is susceptible to renal ischemic damage from an ischemic event; and b) administering to the organism one or more than one effective dose of an agent prior to the ischemic event; where administering to the organism the one or more than one effective dose of the agent serves to at least partially protect the organism's kidney from damage during a subsequent ischemic event. A composition for decreasing renal ischemic damage comprising one or more than one phosphodiesterase inhibitor, and one or more than one HMG-CoA reductase inhibitor.11-27-2008
20090233936Fused Aminopiperidines as Dipeptidyl Peptidase-4 Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-4 enzyme is involved.09-17-2009
20120115875POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY - The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.05-10-2012
20100035887THERAPEUTIC COMPOUNDS FOR BLOCKING DNA SYNTHESIS OF POX VIRUSES - This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.02-11-2010
20090023743INHIBITORS OF PROTEIN KINASES - Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.01-22-2009
20080318966Sinomenine Derivatives and Preparation and Uses Thereof - The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I. The approach disclosed herein is the modification of D ring by-substituting for R. Additional substitutions in the other rings are also provided herein. Several of the sinomenine derivatives have significantly greater anti-inflammation activity when compared with the parent compound.12-25-2008
20080214551Treatment of Burns - The present invention provides methods of treatment of burns, which comprise the step of applying to the burns of a subject a therapeutically effective amount of a metal ion chelating agent.09-04-2008
20090036458ENDOPARASITICIDAL TOPICAL COMPOSITIONS - The present invention provides a composition which comprises: an effective amount of (a) praziquantel and (b) a second endoparasiticidal agent selected from the group consisting of a macrocyclic lactone, imidacloprid and a combination thereof; and (c) 4-allyl-2-methoxyphenol as carrier.02-05-2009
20100267732Prognostic Molecular Markers for ET-743 Treatment - The present invention relates to the use of ecteinascidin 743 in human patients having certain molecular markers profile which has been associated with the outcome of ET-743 chemotherapy. In particular, the invention relates to the use of ecteinascidin 743 in patients having high expression levels of XPG mRNA or protein and/or having a “wild type” genotype for Asp1104His SNP of XPG gene.10-21-2010
20100130505COMPOSITIONS AND METHODS FOR INHIBITING G PROTEIN SIGNALING - Disclosed are compositions and methods for treating diseases associated with G protein βγ subunit activity.05-27-2010
20090253707HETEROANNELATED ANTHRAQUINONE DERIVATIVES AND THE SYNTHESIS METHOD THEREOF - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I):10-08-2009
20100035886PARENTERAL FORMULATIONS OF DOPAMINE AGONISTS - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.02-11-2010
20090291958Substituted PDE5 inhibitors - Provided herein are substituted PDE5 inhibitors of Formula 1, and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function.11-26-2009
20090099191INHIBITION OF NF-KB - The present invention is generally related to the modulation of cell growth or apoptosis. Compositions for modulating cell growth or apoptosis, methods of use thereof, and methods of identification thereof are described.04-16-2009
2011026360816-KETO ASPERGILLIMIDES AND HARMFUL ORGANISM CONTROL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT - Disclosed is a composition for use in controlling ectoparasites, comprising as an active ingredient at least one of compounds represented by formula (I) or (III) or salts thereof. The present invention provides a composition for use in controlling ectoparasites that has excellent ectoparasite control effect and is highly safe.10-27-2011
20100120781Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.05-13-2010
20100120782ENDOPARASITICIDAL GEL COMPOSITION - A homogenous, clear, veterinary gel composition which has a broad spectrum of efficacy against endoparasites over a prolonged period of time and which allows for higher concentrations of a mixture of parasiticidal agents in a single application. This composition is useful for treating and controlling endoparasiticidal infection and infestation in a homeothermic animal.05-13-2010
20100120780TREATMENTS FOR PREMATURE EJACULATION IN HUMANS - Provided are methods and compositions for the treatment of a sexual dysfunction such as premature ejaculation. In certain embodiments, a NMDA antagonist (e.g., dextromethorphan) is administered to a subject in combination with tramadol or a tramadol derivative to treat premature ejaculation. In certain embodiments, a capsaicinoid (e.g., capsaicin) and/or a phosphodiesterase type V inhibitor (e.g., sildenafil citrate) are further administered to the subject. Pharmaceutical preparations such as tablets and capsules are provided.05-13-2010
20100249142IMIDAZOL[1,2-alpha]QUINOXALINES AND DERIVATIVES FOR THE TREATMENT OF CANCERS - Imidazo[1,2-a]quinoxaline compounds for the treatment of cancers as well as pharmaceutical compositions that include these compounds and their uses in therapy.09-30-2010
20100093744THIOGLUCOSE SPIROKETAL DERIVATIVE AND USE THEREOF AS THERAPEUTIC AGENT FOR DIABETES - The present invention provides a compound represented by Formula (II):04-15-2010
20100081664METHOD OF THERAPEUTIC ADMINISTRATION OF DHE TO ENABLE RAPID RELIEF OF MIGRAINE WHILE MINIMIZING SIDE EFFECT PROFILE - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C04-01-2010
20100099687TADALAFIL SOLID COMPOSITES - This invention relates to oral pharmaceutical compositions suitable for making pharmaceutical formulations for oral administration that provide for the rapid dissolution of the phosphodiesterase 5 inhibitor tadalafil. In particular, the pharmaceutical compositions comprise solid composites of tadalafil exhibiting high solubility and rate of dissolution. The invention further relates to methods of preparing these pharmaceutical formulations and the use of such pharmaceutical formulations for treating diseases associated with PDE5 inhibitors.04-22-2010
20100099686COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.04-22-2010
20090042894NOVEL SPECIES OF ACROCARPOSPORA, A METHOD OF PREPARING IODININ, AND THE USES OF IODININ - The present invention provides a novel species of 02-12-2009
20090062292Tetrahydropteridines useful as inhibitors of protein kinases - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.03-05-2009
20100137328TRICYCLIC ANILIDE HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS - Compounds of formula I: wherein variables A06-03-2010
20080280914Intravenous Formulations of Pde Inhibitors - The invention relates to a novel pharmaceutical dosage form of PDE 5 inhibitors for intravenous administration and the use thereof for the treatment of diseases.11-13-2008
20080287450Novel Substituted Tetracyclic Tetahydrofuran, Pyrrolidine And Tetrahydrothiophene Derivatives - This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT11-20-2008
20090318458NOVEL COMPOUNDS AND USE THEREOF - A semiautomatic vehicle gearbox comprising, for said gearbox, a shift lever (12-24-2009
20100267733Synergistic Modulation of Microglial Activation by Nicotine and THC - Treatment of microglial cells with nicotine and THC synergistically attenuate the microglial activation. Using microglial activation, the combination of THC and nicotine interact synergistically reduced LPS induced TNF-α release, showing that the combination of THC and nicotine clinically have greater efficacy in reducing neuroinflammation with less side effects than either drug given alone. CD40 signaling was found critically involved in pathological activation of microglial cells. This invention is also relevant to peripheral inflammation as well thru macrophages. In addition, other cannabinoids and other nicotinic-like medications currently in development are also covered under this discovery.10-21-2010
20080269231Phenazine Compounds and Use Thereof in Autoimmune and Inflammatory Disease - The invention discloses compounds, compositions and methods useful for preventing and/or treating autoimmune diseases and inflammatory diseases. The methods and compositions utilize water-soluble phenazine compounds, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent autoimmune diseases and inflammatory diseases such as those caused by arthritis and rheumatoid arthritis.10-30-2008
20110269764THERAPEUTIC APPROACHES FOR TREATING ALZHEIMER DISEASE AND RELATED DISORDERS THROUGH A MODULATION OF SYNAPSE FUNCTION - The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate synapse function for treating said disease.11-03-2011
20100273803Oral Formulations for Tetrapyrrole Derivatives - Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.10-28-2010
20090181975NEBIVOLOL IN THE TREATMENT OF SEXUAL DYSFUNCTION - The present invention provides methods of treating sexual dysfunction. The methods include administering an effective amount of nebivolol, or a pharmaceutically acceptable salt thereof, alone or in combination with a second active agent e.g. a PDE-5 inhibitor, such as sildenafil citrate. The methods of the present invention are particularly suited to the treatment of erectile dysfunction and female sexual arousal disorder.07-16-2009
20090163507SYNTHESIS OF NATURALLY OCCURING ECTEINASCIDINS AND RELATED COMPOUNDS - Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.06-25-2009
20090143391Aryl and heteroaryl fused imidazo [1,5-a] pyrazines as inhibitors of phosphodiesterase 10 - The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.06-04-2009
20090137599Methods of identifying responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites:dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or fasting triglycerides are greater than about 150 mg/dl and/or said patient has blood pressure of greater than about 135/85 mm Hg. The present invention is also directed to treating identified patients with dopamine agonist therapy.05-28-2009
20090137597Novel quinoxalinone derivatives - A quinoxalinone derivative of the formula (I):05-28-2009
20090143392Methods of Treating Obesity and Metabolic Disorders - The invention relates to methods of treating or preventing obesity, type 2 diabetes, metabolic syndrome, or glucose intolerance using pyrido[3,2-e]pyrazines which are inhibitors of PDE10. The invention further relates to methods of reducing body fat or body weight.06-04-2009
20090143390Parenteral Formulations of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents_useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.06-04-2009
20130217696METHODS FOR THE TREATMENT OF ERECTILE DYSFUNCTION USING FISPEMIFENE - A method of treatment of erectile dysfunction (ED) comprises the step of administering fispemifene to a subject in need thereof in an amount effective to raise the subject's testosterone level. Fispemifene may be used in combination with a PDE-5 inhibitor in individuals who have failed to respond sufficiently to conventional ED treatment. Methods are also disclosed of treating ED by administering clomifene, enclomifene, ospemifene, toremifene and mixtures thereof in combination with a PDE-5 inhibitor.08-22-2013
20090209547C-8 HALOGENATED MACROLIDES - The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof:08-20-2009
20120196869PYRROLOPYRAZINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.08-02-2012
20090247533Ecteinascidins - The present invention is directed to several newly discovered ecteinascidin (Et) species, designated herein as Et 731, Et 815, Et 808, and Et 594. The physical properties of these compounds, their preparation and therapeutic properties are also reported.10-01-2009
20100160334TRICYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: I (where A06-24-2010
20110059977USE OF CANTHIN-6-ONE AND ITS ANALOGS IN THE TREATMENT OF MYCOBACTERIA-LINKED PATHOLOGIES ( amended - The present invention relates to the use, for the preparation of a medicament intended for the treatment or the prevention of pathologies linked to, or caused by mycobacteria, of at least one of the compounds of the following formula (I): in which B represents in particular a nitrogen atom, and R1, R2, R3, R4, R5, R6, R7 and R8 represent in particular a hydrogen atom.03-10-2011
20100210658NOVEL TETRACYCLIC HETEROATOM CONTAINING DERIVATIVES USEFUL AS SEX STEROID HORMONE RECEPTOR MODULATORS - The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.08-19-2010
20090076015Tricyclic Spiro Compound Comprising Acyl Group Bound to Nitrogen Atom in the Ring - It is intended to provide an anticoagulant that has an extremely excellent FXa inhibitory action and an extremely weak hERG channel inhibitory action and can be orally administered, which is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.03-19-2009
20110112105SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SOLID - The present invention relates to toluenesulfonic acid addition salt crystals of specific substituted heterocycle fused gamma-carbolines, the method of making and using such crystals.05-12-2011
20100197695ANTITUMORAL DERIVATIVES OF ET-743 - Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula Ia.:08-05-2010
20090318459Therapeutic Compositions Comprising a Specific Endothelin Receptor Antagonist and a PDE5 Inhibitor - The invention relates to a product containing the compound of formula (I) below12-24-2009
20090137598METHOD OF TREATING METABOLIC DISORDERS AND DEPRESSION WITH DOPAMINE RECEPTOR AGONISTS - This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant.05-28-2009
20090318460AMORPHOUS VARENICLINE TARTRATE AND PROCESS FOR THE PREPARATION THEREOF - The present invention generally relates to an amorphous form of varenicline and its pharmaceutically acceptable salts thereof. More particularly the present invention relates to amorphous forms of varenicline and its L-tartrate salt; a process for their preparation and pharmaceutical compositions comprising the same.12-24-2009
20090111818Combinations of Eszopiclone and O-Desmethylvenlafaxine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is O-desmethylvenlafaxine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.04-30-2009
20080287451Method of therapeutic administration of DHE to enable rapid relief of migraine while minimizing side effect profile - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C11-20-2008
20110130405SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS - This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.06-02-2011
20110112106TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.05-12-2011
20130137697COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT - Briefly described, embodiments of this disclosure, among others, include compositions, pharmaceutical compositions, methods of treating nicotine dependence, methods of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorder, method of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorders, and the like.05-30-2013
20130137698SOLID ORAL FILM DOSAGE FORMS AND METHODS FOR MAKING SAME - Improved pharmaceutical solid oral film dosage forms for the buccal and/or sublingual delivery of pharmaceutical, nutraceutical or cosmetic ingredients are endowed with instant hydration potential and complete dissolution potentially enabling the active ingredient to become immediately available for enhanced buccal and/or sublingual absorption and/or reduced absorption through the gastrointestinal route. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced stability by the use of a combination of crystallization inhibitors, which together can maintain the active ingredient in a desired plurality of particles in an effective size range within a polymeric film matrix.05-30-2013
20100324055SOLID STATES FORMS OF VARENICLINE SALTS AND PROCESSES FOR PREPARATION THEREOF - Salts and crystalline forms of several salts of Varenicline, i.e., Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, methods of preparing the solid states of Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, and processes for preparing Varenicline base from those Varenicline salts are provided.12-23-2010
20110245261ANTIPROLACTINIC VETERINARY COMPOSITION FOR RUMINANTS - This present invention relates to an antiprolactinic veterinary composition to be administered to ruminants. Said composition comprises at least one antiprolactinic compound which is an agonist of dopamine receptors, and is particularly useful for promoting a substantial reduction of lactation, mammary involution, and for treating and/or intra-mammary diseases or infections of ruminants.10-06-2011
20110034471NOVEL COMBINATIONS COMPRISING A PHOSHODIESTERASE-5 INHIBITOR AND THEIR USE - The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.02-10-2011
20110034473NOVEL (PYRROLOQUINOXALINYL) PYRAZINECARBOHYDRAZIDE-OXALIC ACID CO-CRYSTAL FOR TREATMENT OF CANCER AND OTHER DISEASES - A novel co-crystal of N′-(7-fluoropyrrolo[1,2a]quinoxalin-4-yl)pyrazine-2-carbohydrazide with oxalic acid is disclosed. The disclosed oxalic acid co-crystal demonstrates cancer cell growth inhibition and is more bioavailable than the corresponding free base when administered as a suspension.02-10-2011
20110034472Novel Compounds for Treatment of Cancer and Disorders Associated With Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.02-10-2011
20100222357INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES - The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I:09-02-2010
20110245260ANALOGS OF DEHYDROPHENYLAHISTINS AND THEIR THERAPEUTIC USE - Compounds represented by the following structure (II) are disclosed:10-06-2011
20090215786NOVEL CYSTEINE PROTEASE INHIBITORS AND THEIR THERAPEUTIC APPLICATIONS - The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.08-27-2009
20110082150Headache pre-emption by dihydroergotamine treatment during headache Precursor events - Disclosed are methods that address providing a subject experiencing, or who has experienced, a headache precursor event and administering dihydroergotamine, or a pharmaceutically acceptable salt or complex thereof, to the subject by oral inhalation, in an amount effective to pre-empt a subsequent headache in the subject. Also disclosed are compositions that are related to those methods.04-07-2011
20110071155Tricyclic Nitrogen Containing Compounds And Their Use As Antibacterials - Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof:03-24-2011
20090030006SPIROKETAL DERIVATIVES AND USE THEREOF AS DIABETIC MEDICINE - The present invention provides a compound of Formula (I):01-29-2009
20110152280NOVEL ERGOLINE ANALOGS - Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT06-23-2011
20120202821CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS - Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT08-09-2012
20080269230Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders - This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH.10-30-2008
20080255132Combination Therapy Comprising the Use of Et-743 and Paclitaxel for Treating Cancer - Methods of treating a human body for cancer are provided. In one aspect, an effective therapeutic amount of paclitaxel is administered in combination with ET-743 in a dose range between 0.5 and 1 mg/m10-16-2008
20110053947Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof - The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.03-03-2011
20110263607ALPHA HELIX MIMETICS IN THE TREATMENT OF CANCER - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.10-27-2011
20110263606SOLID ORAL DOSAGE FORMS COMPRISING TADALAFIL - Improved pharmaceutical solid oral dosage forms for the buccal and/or sublingual delivery of Tadalafil. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced methods of preparation by the use improved solubilization systems which can maintain the Tadalafil in a buccal and/or sublingual oral dosage form or a polymeric film matrix that provides improved bioavailability and/or absorption of Tadalafil.10-27-2011
20100168119COMPOSITIONS AND METHODS FOR MINIMIZING OR REDUCING AGONIST-INDUCED DESENSITIZATION - Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.07-01-2010
20110082151SULFONYLUREA MODULATORS OF ENDOTHELIN RECEPTOR - The present invention relates to new sulfonylurea modulators of endothelin receptor activity, pharmaceutical compositions thereof, and methods of use thereof.04-07-2011
20090298842Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor - Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases. Additionally disclosed are novel 4,5,6,7-tetrahydrobenzo[b]thiophene compounds, benzo(g)quinoxaline compounds, and pharmaceutically acceptable salts thereof, and methods of using such compounds and salts thereof for the prophylaxis and/or treatment of virally and/or bacterially induced infections, particularly mycobacteria-induced infections, including opportunistic infections, as well as pharmaceutical compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene compound and/or benzo(g)quinoxaline compound and/or pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier.12-03-2009
20110136817Methods of identifying responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites:dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or fasting triglycerides are greater than about 150 mg/dl and/or said patient has blood pressure of greater than about 135/85 mm Hg. The present invention is also directed to treating identified patients with dopamine agonist therapy.06-09-2011
20100029666Macrocyclic Quinoxaline Compounds as HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections.02-04-2010
20100029665Methods and Compositions for Treating Migraine Pain - The present invention provides novel methods and compositions for the treatment and prevention of headaches, vascular headaches, migraine headaches, cluster headaches, and migraine. One of the headaches, vascular headaches, migraine headaches, cluster headaches, and migraine treated by the methods and compositions of the invention is migraine.02-04-2010
20120040990INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES - The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I:02-16-2012
20100179159METHOD FOR THE PRODUCTION OF A MEDICAMENT CONTAINING TADALAFIL - The invention relates to a method for producing a medicament containing tadalafil. In said method, tadalafil is mixed with suitable adjuvants and is heated to a temperature of about 100° C. to about 200° C., preferably about 150° C. to about 200° C., especially about 200° C.07-15-2010
20090042895Antidepressant Piperidine Derivatives of Heterocycle-Fused Benzodioxans - Compounds of the Formula:02-12-2009
20090215787Preparations of new polymorphic forms of varenicline tartrate - The present invention is directed to an amorphous form, three novel polymorph form of crystalline varenicline tartrate, namely Form D, Form E and Form F. The present invention also provides processes of their preparations and pharmaceutical composition comprising such material and their use in therapy. Form D is new anhydrous varenicline tartrate, and can be prepared from recrystallizing varenicline tartrate in a mixture of methanol and water or a mixture of N,N-dimethylformamide and water. Form E is a new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of isopropanol and water. Form F is another new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of acetone and water. The X-ray powder diffraction pattern (X-RPD), Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) techniques are used to characterize amorphous form and crystalline polymorphic forms.08-27-2009
20110086859ALKYL SUBSTITUTED INDOLOQUINOXALINES - Novel substituted indoloquinoxalines of formula (I04-14-2011
20090312338Novel Tricyclic Compounds - The invention provides a compound of Formula (I)12-17-2009
20120178760Heterocyclic-Fused Pyrazolo[4,3-c] Pyridin-3-One M1 Receptor Positive Allosteric Modulators - The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.07-12-2012
20120178759CONDENSED PYRIDINE DERIVATIVES USEFUL AS POTENT INHIBITORS OF THE PROTEIN KINASE CK2 - The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen Camongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy.07-12-2012
20090076016FORMULATIONS COMPRISING JORUMYCIN-, RENIERAMYCIN-, SAFRACIN- OR SAFRAMYCIN-RELATED COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES - Jorumycin, renieramycin, safracin and saframycin related compounds formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.03-19-2009
20110112104TRICYCLIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. - Compounds of formula (I):05-12-2011
20100179158INHIBITORS OF CYCLIC AMP PHOSPHODIESTERASES - Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders.07-15-2010
20110105517THERAPEUTIC AGENT FOR AMYOTROPHIC LATERAL SCLEROSIS - Disclosed is a safe and effective therapeutic agent that can alleviate the symptoms of the intractable disease ALS and slow the progress thereof. The therapeutic agent for amyotrophic lateral sclerosis contains bromocriptine or a pharmaceutically acceptable salt thereof as the active ingredient.05-05-2011
20110105516POLYMERIZED MICELLES - Polymerised micelles comprising polymerised amphiphilic molecules obtained starting from amphiphilic molecules having one or two lipid chains each comprising one or two polymerisable moieties and linked to a polar head.05-05-2011
20110105515TARGETING THE ONCOPROTEIN NUCLEOPHOSMIN - (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin.05-05-2011
20120046297CRYSTALIZATION OF PHARMACEUTICAL COMPOUNDS - Novel crystalline forms of tadalafil suitable for pharmaceutical compositions in drug delivery systems for humans.02-23-2012
20120004240INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.01-05-2012
20120004239 Process for Preparing Quinoxaline Derivatives - The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof.01-05-2012
20090170860Use of PARP-1 Inhibitors - A method for improving the cytotoxic effect of Ecteinascidin-743 (ET-743) or an analog thereof on a tumor cell population in a patient the method including administering to the patient, sequentially or simultaneously, a therapeutically effective combination of a composition including ET-743 and an amount of a composition including a PARP-1 inhibitor effective to increase the cytotoxic effect of ET-743 on the tumor cell population. Anti-tumor compositions containing a therapeutically effective amount of ET-743 and an amount of a PARP-1 inhibitor effective to increase the tumor cytotoxicity of the ET-743 are also presented.07-02-2009
20120015953METHODS AND COMPOSITIONS FOR THE TREATMENT OF ALLERGY - The present invention relates to compositions comprising an antagonist of the histamine H1 receptor and a compatible antagonist of the histamine H4 receptor. The antagonist compounds are selected to prevent the H4 receptor antagonist from interfering with the H1 receptor antagonist's suppression of acute phase allergic responses in a patient. The present invention also relates to compositions comprising a mast cell stabilizer and a compatible antagonist of the histamine H4 receptor.01-19-2012
20120157460TETRAHYDRO-AZACARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF - The present invention relates to tetrahydro-azacarboline derivatives of formula (I):06-21-2012
20120071484Topical Parasiticide Composition - A topical parasiticide composition comprising: (i) a phenyl pyrazole insecticide; and/or a neonicotinoid; (ii) a macrocylic lactone and/or an aminoacetonitrile derivatives; (iii) an Insect Growth Regulator; and (iv) a 2-acyl-4-oxo-1,2,3,6,7,11b-4H-pyrazino[2,1a]isoquinoline derivative.03-22-2012
20110092511INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.04-21-2011
20120157461Indolyl-Substituted Pyrazino-Quinolines and Their Use for the Treatment of Cancer - There is provided compounds of formula I, wherein the wedged bonds, R06-21-2012
20110065715Nogo Receptor Binding Small Molecules to Promote Axonal Growth - The present invention provides a method for identifying compounds which modulate the interaction of Nogo and Nogo receptor (NgR). The present invention also provides compounds that modulate the interaction of Nogo and Nogo receptor (NgR), the use of such compounds and compositions in the treatment or amelioration of conditions diseases or disorders, such as spinal cord injury, traumatic brain injury, stroke, multiple sclerosis, ALS, Huntington's disease, Alzheimer's disease, Parkinson's disease, epilepsy, Schizophrenia or schizoaffective disorders.03-17-2011
20120122879COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.05-17-2012
20120135998COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS - The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds.05-31-2012
20120122878COMBINATION PRODUCTS - The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.05-17-2012
20080234279Ecteinascidins - The present invention is directed to several newly discovered ecteinascidin (Et) species, designated herein as Et 731, Et 815, Et 808, and Et 594. The physical properties of these compounds, their preparation and therapeutic properties are also reported.09-25-2008
20120232086FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY - The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R09-13-2012
201202320853,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.09-13-2012
20120172367MACROCYCLIC INTEGRASE INHIBITORS - Compound having formula (I), wherein —W is NH—, —N(CH07-05-2012
20100009999ALKYL SUBSTITUTED INDOLOQUINOXALINES - Novel substituted indoloquinoxalines of formula (I01-14-2010
20080300253TREATMENT OF INFLAMMATORY DISORDERS WITH PRAZIQUANTEL - Methods of treating and/or preventing disorders mediated by one or more of TNF-α, NF-κB, IKK-α, IKK-β, ATF-2 and p38 kinase by administration of praziquantel, or a pharmaceutically acceptable salt, prodrug, ester or amide thereof. These disorders include inflammatory disorders such as autoimmune diseases.12-04-2008
20090209546L-Malate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-- Dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.08-20-2009
20100190799PHENAZINE COMPOUNDS AND USE THEREOF IN AUTOIMMUNE AND INFLAMMATORY DISEASES - The invention discloses compounds, compositions and methods useful for preventing and/or treating autoimmune diseases and inflammatory diseases. The methods and compositions utilize water-soluble phenazine compounds, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent autoimmune diseases and inflammatory diseases such as those caused by arthritis and rheumatoid arthritis.07-29-2010
20120270881CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS - Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y10-25-2012
20100249143METHOD FOR INHIBITING GROWTH OF CANCER CELLS AND CELL TELOMERE AND DISEASES OF CELL PROLIFERATION BY USING HETEROANNELATED ANTHRAQUINONE DERIVATIVE COMPOUNDS - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I):09-30-2010
20100234388SUBSTITUTED PDE5 INHIBITORS - Provided herein are substituted PDE5 inhibitors of Formula (1), and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function. The compounds are deuterated tadalafil derivatives.09-16-2010
20120329806NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT12-27-2012
20100204239NOVEL TETRACYCLIC HETEROATOM CONTAINING DERIVATIVES USEFUL AS SEX STEROID HORMONE RECEPTOR MODULATORS - The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.08-12-2010
20120149709PYRAZINOISOQUINOLINE COMPOUNDS - This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.06-14-2012
20110160219Inhibitors of Phosphodiesterase Type 5A for Treating or Preventing Muscle Disease or the Symptoms Thereof in a Patient - Disclosed are pharmaceutical compositions and methods for treating or preventing muscle diseases or the symptoms thereof. The compositions typically include and the methods typically utilize phosphodiesterase type 5A inhibitors.06-30-2011
20110160218COMPOSITIONS COMPRISING MACROCYCLIC LACTONE COMPOUNDS AND SPIRODIOXEPINOINDOLES - The present invention provides formulations which may comprise macrocyclic lactones and at least one spirodioxepinoindole derivative or a spirooxepinoindole derivative for combating parasites in birds and mammals. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.06-30-2011
20110160217DEUTERIUM ENRICHED ANALOGUES OF TADALAFIL AS PDE5 INHIBITORS - The present invention relates to derivatives of tadalafil, substituted with fluorine on the methylene carbon atom situated between the oxygens of the benzodioxol ring, and optionally further substituted with deuterium atoms in place of normally abundant hydrogen, and 06-30-2011
20130172361ASSAYS AND METHODS FOR SELECTING A TREATMENT REGIMEN FOR A SUBJECT WITH DEPRESSION - Disclosed herein are novel assays, systems and kits for selecting a treatment regimen for a subject with depression by identifying at least one nucleic acid polymorphism, e.g., but not limited to, at the MTHFR, MTR, or MTRR locus, and/or determining expression levels of peripheral biomarkers (e.g., SAM, SAH, and 4-HNE) in a test sample from a human subject. These biomarkers can be used to determine the effectiveness of treating a depressed subject with a folate-containing compound (alone or as an adjunct to an antidepressant). Additionally, these biomarkers can be used to select an appropriate treatment regimen for subjects with treatment-resistant depression (e.g., resistant to at least one selective serotonin reuptake inhibitor). Methods and compositions for treating a subject with depression and/or determining or improving the effectiveness of an antidepressant drug taken by a subject are also provided herein.07-04-2013
20130116262BICYCLIC PIPERAZINE COMPOUNDS - Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.05-09-2013
20090076017DEUTERIUM-ENRICHED TRABECTEDIN - The present application describes deuterium-enriched trabectedin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090239873Phenyl-piperazine derivatives as modulators of muscarinic receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.09-24-2009
20110224218METHOD FOR INHIBITING GROWTH OF CANCER CELLS AND CELL TELOMERE AND DISEASES OF CELL PROLIFERATION BY USING HETEROANNELATED ANTHRAQUINONE DERIVATIVE COMPOUNDS - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (IV):09-15-2011
20110275646Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression.11-10-2011
20110275645Small Molecules for Inhibition of Protein Kinases - The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.11-10-2011
20110237597METHOD OF TREATING PERIPHERAL NERVE SENSORY LOSS USING COMPOUNDS HAVING NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVITY - Methods for treatment of peripheral nerve sensory loss are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.09-29-2011
20130197005Parenteral Formulations Of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.08-01-2013
20130197006Non-Starch Based Soft Chewables - The present invention generally relates to soft chewables, especially suitable for delivering active ingredients to animals and processes for the preparation thereof. In various embodiments, the soft chewable comprises a pharmaceutically effective amount of at least one active ingredient, a flavoring agent, a disintegrant a humectant, an antioxidant, a preservative, and water. In accordance with preferred embodiments, the soft chewable is essentially free of starch, oil glycols, waxes, and soy products.08-01-2013
20130203762VETERINARY ANTIPROLACTINIC COMPOSITION FOR RUMINANTS - This present invention relates to an antiprolactinic veterinary composition to be administered to ruminants. Said composition comprises at least one antiprolactinic compound which is an agonist of dopamine receptors, and is particularly useful for reducing udder engorgement and/or the reduction of pain after drying off and/or of increasing welfare, and/or of reducing milk leakage in ruminants as well as for preventing new mammary microbial infections, secondary infection, or co-infections in ruminants and mastitis.08-08-2013
20120088774ACTIVE PHARMACEUTICAL INGREDIENT ADSORBED ON SOLID SUPPORT - The present invention belongs to the field of pharmaceutical industry and relates to dosage forms comprising active pharmaceutical ingredients (API) such as tadalafil, simvastatin, fenofibrate and lovastatin that are practically insoluble in water, adsorbed on a carrier. Furthermore it relates to an adsorbate comprising API being practically insoluble in water and to a process for the preparation of said adsorbate with non-polar solvent (s) such as chlorinated hydrocarbon, diisopropylethes and hexane. Furthermore the invention relates to a process for the preparation of the dosage form, as well as to the use of the adsorbate for the preparation of the dosage form. Moreover it relates to the dosage form for use in the treatment of erectile dysfunction, human immunodeficiency virus (HIV) infections and/or Acquired Immune Deficiency Syndrome (AIDS).04-12-2012
20120088773Circadian rhythm modulation - A method and composition is herein described to modulate the circadian rhythm to effect summer metabolism and the metabolic syndrome. The method entails the once daily, timed ingestion of a dopamine precursor or a dopamine agonist, receptor primed with caffeine, and vitamin D04-12-2012

Patent applications in class At least three rings in the polycyclo ring system

Patent applications in all subclasses At least three rings in the polycyclo ring system